CN101220071B - 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 - Google Patents
稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 Download PDFInfo
- Publication number
- CN101220071B CN101220071B CN2008100192275A CN200810019227A CN101220071B CN 101220071 B CN101220071 B CN 101220071B CN 2008100192275 A CN2008100192275 A CN 2008100192275A CN 200810019227 A CN200810019227 A CN 200810019227A CN 101220071 B CN101220071 B CN 101220071B
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- China
- Prior art keywords
- guanine nucleoside
- stable
- methoxyl group
- dideoxy
- dideoxy guanine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- UYTPUPDQBNUYGX-UHFFFAOYSA-N Guanine Natural products O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 title claims description 55
- -1 guanine nucleoside Chemical class 0.000 title claims description 55
- 239000000203 mixture Substances 0.000 title claims description 11
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- 239000000825 pharmaceutical preparation Substances 0.000 description 4
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- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 2
- 241000700605 Viruses Species 0.000 description 2
- ARLKCWCREKRROD-POYBYMJQSA-N [[(2s,5r)-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)CC1 ARLKCWCREKRROD-POYBYMJQSA-N 0.000 description 2
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- OCLZPNCLRLDXJC-NTSWFWBYSA-N 2-amino-9-[(2r,5s)-5-(hydroxymethyl)oxolan-2-yl]-3h-purin-6-one Chemical group C1=2NC(N)=NC(=O)C=2N=CN1[C@H]1CC[C@@H](CO)O1 OCLZPNCLRLDXJC-NTSWFWBYSA-N 0.000 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 102000016928 DNA-directed DNA polymerase Human genes 0.000 description 1
- 108010014303 DNA-directed DNA polymerase Proteins 0.000 description 1
- 241000725618 Duck hepatitis B virus Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 229940124872 Hepatitis B virus vaccine Drugs 0.000 description 1
- 241000701076 Macacine alphaherpesvirus 1 Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
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- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 1
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- 230000005764 inhibitory process Effects 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 description 1
- 229960001627 lamivudine Drugs 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
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- 150000003833 nucleoside derivatives Chemical class 0.000 description 1
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- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
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- 239000001226 triphosphate Substances 0.000 description 1
- 235000011178 triphosphate Nutrition 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Biotechnology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100192275A CN101220071B (zh) | 2008-01-17 | 2008-01-17 | 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 |
| PCT/CN2008/072646 WO2009089702A1 (fr) | 2008-01-17 | 2008-10-10 | 6-méthoxy-2',3'-didésoxyguanosine stable, son procédé de préparation et composition pharmaceutique la contenant |
| JP2010542498A JP5940245B2 (ja) | 2008-01-17 | 2008-10-10 | 安定な６‐メトキシ‐２’、３’‐ジデオキシグアノシン及びその製造方法、並びにそれを含む医薬組成物 |
| US12/743,898 US8349811B2 (en) | 2008-01-17 | 2008-10-10 | Stable 6-methoxy-2′,3′-dideoxyguanosine, method for preparing the same and pharmaceutical composition containing the same |
| EP08871110.6A EP2241571B1 (en) | 2008-01-17 | 2008-10-10 | A process for the preparation of 6-methoxy-2',3'-dideoxyguanosine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100192275A CN101220071B (zh) | 2008-01-17 | 2008-01-17 | 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101220071A CN101220071A (zh) | 2008-07-16 |
| CN101220071B true CN101220071B (zh) | 2011-04-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008100192275A Active CN101220071B (zh) | 2008-01-17 | 2008-01-17 | 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8349811B2 (enrdf_load_html_response) |
| EP (1) | EP2241571B1 (enrdf_load_html_response) |
| JP (1) | JP5940245B2 (enrdf_load_html_response) |
| CN (1) | CN101220071B (enrdf_load_html_response) |
| WO (1) | WO2009089702A1 (enrdf_load_html_response) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101220071B (zh) | 2008-01-17 | 2011-04-06 | 南京长澳医药科技有限公司 | 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 |
| CN102552158B (zh) * | 2010-12-22 | 2016-04-27 | 广州一品红制药有限公司 | 美他卡韦肠溶微丸及其制备方法 |
| CN102070691B (zh) * | 2010-12-22 | 2012-09-19 | 南京长澳医药科技有限公司 | 一种美他卡韦晶型,其制备方法以及包含它的药物组合物 |
| CN103360448A (zh) * | 2012-04-09 | 2013-10-23 | 南京长澳医药科技有限公司 | 美他卡韦乙醇溶剂化合物的单晶晶型，及制备方法 |
| WO2014168947A2 (en) * | 2013-04-08 | 2014-10-16 | The Board Of Regents Of The University Of Texas System | Telomerase mediated telomere altering compounds |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0286028A2 (de) * | 1987-04-10 | 1988-10-12 | Roche Diagnostics GmbH | Desaza-purin-nucleosid-Derivate, Verfahren zu deren Herstellung sowie deren Verwendung bei der Nucleinsäure-Sequenzierung sowie als antivirale Mittel |
| EP0286425A2 (en) * | 1987-04-09 | 1988-10-12 | The Wellcome Foundation Limited | Therapeutic nucleosides |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5185437A (en) * | 1987-04-09 | 1993-02-09 | Burroughs Wellcome Co. | Therapeutic nucleosides |
| WO1990006312A1 (de) | 1988-11-29 | 1990-06-14 | Institut Für Molekularbiologie Und Analytik (Ima) Gmbh | 2', 3'-didesoxyribofuranoside und ein verfahren zu ihrer herstellung |
| PT95516A (pt) * | 1989-10-06 | 1991-08-14 | Wellcome Found | Processo para a preparacao de derivados de 2',3'-didesoxi nucleosidos 6-substituidos |
| CN1309732C (zh) | 2002-10-28 | 2007-04-11 | 南京长澳医药科技有限公司 | 6－烷氧基－2’，3’－双脱氧鸟嘌呤核苷的制备方法 |
| CN1293884C (zh) | 2002-10-29 | 2007-01-10 | 南京长澳医药科技有限公司 | 6－甲氧基双脱氧鸟苷在制备抗乙肝药物中的应用 |
| CN101147728A (zh) | 2007-10-26 | 2008-03-26 | 中国药科大学 | 6-甲氧基双脱氧鸟苷长循环脂质体制剂及制备方法 |
| CN101220071B (zh) | 2008-01-17 | 2011-04-06 | 南京长澳医药科技有限公司 | 稳定的6-甲氧基-2’,3’-双脱氧鸟嘌呤核苷及其制备方法和包含它的药物组合物 |
-
2008
- 2008-01-17 CN CN2008100192275A patent/CN101220071B/zh active Active
- 2008-10-10 JP JP2010542498A patent/JP5940245B2/ja active Active
- 2008-10-10 US US12/743,898 patent/US8349811B2/en active Active
- 2008-10-10 WO PCT/CN2008/072646 patent/WO2009089702A1/zh active Application Filing
- 2008-10-10 EP EP08871110.6A patent/EP2241571B1/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0286425A2 (en) * | 1987-04-09 | 1988-10-12 | The Wellcome Foundation Limited | Therapeutic nucleosides |
| EP0286028A2 (de) * | 1987-04-10 | 1988-10-12 | Roche Diagnostics GmbH | Desaza-purin-nucleosid-Derivate, Verfahren zu deren Herstellung sowie deren Verwendung bei der Nucleinsäure-Sequenzierung sowie als antivirale Mittel |
Non-Patent Citations (1)
| Title |
|---|
| Morris J. Robins, et al.Nucleic Acid Related Compounds. 114. Synthesis of 2,6-(Disubstituted)purine 2",3"-Dideoxynucleosides and Selected Cytotoxic, Anti-Hepatitis B, and Adenosine Deaminase Substrate Activities.《Journal of Heterocyclic Chemistry》.2001,第38卷1297-1306. * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP5940245B2 (ja) | 2016-06-29 |
| JP2011509946A (ja) | 2011-03-31 |
| EP2241571A4 (en) | 2012-01-25 |
| US8349811B2 (en) | 2013-01-08 |
| WO2009089702A1 (fr) | 2009-07-23 |
| EP2241571A1 (en) | 2010-10-20 |
| CN101220071A (zh) | 2008-07-16 |
| EP2241571B1 (en) | 2017-01-18 |
| US20100311681A1 (en) | 2010-12-09 |
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Effective date of registration: 20221111 Address after: No.6 Dongbo Road, East District, Guangzhou Economic and Technological Development Zone, Guangdong 510000 Patentee after: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. Patentee after: GUANGDONG ZERUI PHARMACEUTICAL Co.,Ltd. Patentee after: Guangzhou Lianrui Pharmaceutical Co.,Ltd. Patentee after: Guangzhou Runlin Pharmaceutical Technology Co.,Ltd. Patentee after: Euphorbia Biological Medicine Co.,Ltd. Address before: 510760 Building 1, No.6 Dongbo Road, Guangzhou Economic and Technological Development Zone, Guangzhou City, Guangdong Province Patentee before: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. |
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| TR01 | Transfer of patent right | ||
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Effective date of registration: 20221221 Address after: No.6 Dongbo Road, East District, Guangzhou Economic and Technological Development Zone, Guangdong 510000 Patentee after: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. Patentee after: GUANGDONG ZERUI PHARMACEUTICAL Co.,Ltd. Patentee after: Guangzhou Lianrui Pharmaceutical Co.,Ltd. Patentee after: Guangzhou Runlin Pharmaceutical Technology Co.,Ltd. Patentee after: Euphorbia Biological Medicine Co.,Ltd. Patentee after: Guangdong Ruishi Pharmaceutical Technology Co.,Ltd. Address before: No.6 Dongbo Road, East District, Guangzhou Economic and Technological Development Zone, Guangdong 510000 Patentee before: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. Patentee before: GUANGDONG ZERUI PHARMACEUTICAL Co.,Ltd. Patentee before: Guangzhou Lianrui Pharmaceutical Co.,Ltd. Patentee before: Guangzhou Runlin Pharmaceutical Technology Co.,Ltd. Patentee before: Euphorbia Biological Medicine Co.,Ltd. |